{"title":"Amphibian-Derived Antimicrobial Peptides: Essential Components of Innate Immunity and Potential Leads for New Antibiotic Development.","authors":"Ebru Tanriverdi O","doi":"10.2174/0109298665356946241218103145","DOIUrl":"10.2174/0109298665356946241218103145","url":null,"abstract":"<p><p>Like other vertebrates, amphibians possess innate and adaptive immune systems. At the center of the adaptive immune system is the Major Histocompatibility Complex. The important molecules of innate immunity are antimicrobial peptides (AMPs). These peptides are secreted by granular glands in the skin and protect the animal against microorganisms entering its body through the skin. AMPs offer an effective and rapid defense against pathogenic microorganisms and have cationic and amphiphilic structures. These peptides are small gene-encoded molecules of 8-50 amino acid residues synthesized by ribosomes. These small molecules typically exhibit activity against bacteria, viruses, fungi, and even cancer cells. It is known that today's amphibian AMPs originated from a common precursor gene 150 million years ago and that the origin of these peptides is preprodermaseptins. Today, antibiotic resistance has occurred due to the incorrect use of antibiotics. Traditional antibiotics are becoming increasingly inadequate. AMPs are considered promising candidates for the development of new-generation antibiotics. Therefore, new antibiotic discoveries are needed. AMPs are suitable molecules for new-generation antibiotics that are both fast and have different killing mechanisms. One of the biggest problems in the clinical applications of AMPs is their poor stability. AMPs generally have limited tropical applications because they are sensitive to protease degradation. Coating these peptides with nanomaterials to make them more stable can solve this problem.</p>","PeriodicalId":20736,"journal":{"name":"Protein and Peptide Letters","volume":" ","pages":"97-110"},"PeriodicalIF":1.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142953978","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Evaluation of Anti-cancer Potential of <i>Abelmoschus esculentus</i> (Okra).","authors":"Maanniya Gakhar, Lovepreet Singh, Sanjeev Routh, Arunika Mukhopadhaya, Desh Deepak Singh","doi":"10.2174/0109298665365981250801110725","DOIUrl":"10.2174/0109298665365981250801110725","url":null,"abstract":"<p><strong>Introduction: </strong>Abelmoschus esculentus (okra) from the Malvaceae family is widely used in culinary applications and is reported to have many potential therapeutic effects attributed to the compounds isolated from it. In this work, we set out to explore its seed proteome for the isolation of lectins and characterize them.</p><p><strong>Methods: </strong>A protein of about 21kDa was isolated and purified using chromatography techniques from the ammonium sulphate crude protein extract. It was evaluated for hemagglutination activity on rabbit erythrocyte suspension, trypsin inhibitory activity using chemical assay, and evaluation of anti-cancer activity using cell lines. Mass and transcriptome analysis were done to deduce the complete sequence of the isolated protein.</p><p><strong>Results: </strong>Using functional, mass, and transcriptome analysis, the protein was identified as AEL (Abelmoschus esculentus lectin), which was reported earlier. Only a partial sequence of AEL was known, and in this work, we have deduced its complete sequence. It showed significant anti-- cancer activity against HeLa (cervical cancer) and T84 (colon cancer) with MIC (Minimum inhibitory concentration) of 20μg/ml and 40% and 30% reduction in cell viability at 100μg/ml and insignificant effect on ACHN (adenocarcinoma) cell lines. No significant effect was seen with the tested doses on normal control human cell lines HEK293 (human embryonic kidney cells). The purified protein shows specificity for lactose and galactose in the hemagglutination assay and trypsin inhibition activity.</p><p><strong>Discussion: </strong>Studies of okra seed proteome lead to purification of AEL, a 21 kDa protein with dual hemagglutination activity and trypsin inhibitory activity. It showed potential anticancer activity in cervical, colon cancer cell lines and minimal effects on adenocarcinoma and control cell lines, suggesting specificity. The complete sequence of AEL was elucidated which will aid in its bioinformatics analysis.</p><p><strong>Conclusion: </strong>There are very few reported dual-acting lectins with potential anticancer activity, and this work will help understand their mechanistic interactions better.</p>","PeriodicalId":20736,"journal":{"name":"Protein and Peptide Letters","volume":" ","pages":"575-583"},"PeriodicalIF":1.1,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144966262","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"PLEKHG7 Expression: A Biomarker for Prognosis and Targeted Therapy in Diffuse Large B-cell Lymphoma.","authors":"Guizhen Lyu, Dongbing Li","doi":"10.2174/0109298665398122250929045705","DOIUrl":"10.2174/0109298665398122250929045705","url":null,"abstract":"<p><strong>Introduction: </strong>Pleckstrin homology and RhoGEF domain-containing G7 (PLEKHG7) is a largely uncharacterized gene whose role in diffuse large B-cell lymphoma (DLBCL) remains unexplored. Thus, we aimed to profile PLEKHG7 expression, assess its prognostic value, and explore therapeutic implications.</p><p><strong>Methods: </strong>RNA-seq data from TCGA-DLBCL (n=48) and GTEx normal tissues were analyzed via UCSC XENA. Differential expression was tested using the Wilcoxon rank-sum test and FDR correction. Prognostic significance was evaluated by Kaplan-Meier and multivariate Cox regression (nomogram). Gene set enrichment analysis (GSEA) mapped PLEKHG7-associated pathways. Drug sensitivity correlations were extracted from RNAactDrug. qRT-PCR validated expression in DLBCL cell lines (OCI-Ly3, SU-DHL-4) versus normal B lymphocytes (GM12878).</p><p><strong>Results: </strong>PLEKHG7 was markedly up-regulated in DLBCL tissues (P < 0.001) and cell lines versus normal controls (AUC = 0.739). High PLEKHG7 expression predicted inferior overall survival (HR = 8.88; 95% CI: 1.09-72.27; P = 0.041) and remained an independent prognostic factor (HR = 10.109; P = 0.033). GSEA linked PLEKHG7 to ribosome, oxidative phosphorylation, proteasome, cytokine-cytokine receptor interaction, spliceosome, and ECM-receptor pathways. Elevated PLEKHG7 negatively correlated with sensitivity to idelalisib, omipalisib, belinostat, methotrexate, and dacinostat.</p><p><strong>Discussion: </strong>The study's limitations include reliance on bioinformatics data and the lack of functional validation. Further research is needed to elucidate the molecular mechanisms underlying PLEKHG7's role in DLBCL and validate its clinical utility.</p><p><strong>Conclusion: </strong>PLEKHG7 is significantly overexpressed in DLBCL and independently predicts poor prognosis. Its association with key oncogenic pathways and drug resistance underscores its potential as both a prognostic biomarker and a therapeutic target, warranting further functional validation.</p>","PeriodicalId":20736,"journal":{"name":"Protein and Peptide Letters","volume":" ","pages":"657-666"},"PeriodicalIF":1.1,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145233283","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Recombinant Expression of L-methioninase from <i>Brevibacterium linens</i> and Evaluation of its Anticarcinogenic Properties against MiaPaCa-2 Cells.","authors":"Semih Latif Ipek, Meryem Damla Ozdemir Alkıs, Ahmet Tulek, Dilek Gokturk","doi":"10.2174/0109298665383781250624054915","DOIUrl":"10.2174/0109298665383781250624054915","url":null,"abstract":"<p><strong>Introduction: </strong>This study aimed to investigate the anti-carcinogenic effects of recombinant L- methioninase (rBlmet) on the pancreatic cancer cell line MiaPaCa-2.</p><p><strong>Methods: </strong>In this study, rBlmet was initially cloned, expressed, and purified. To increase enzyme activity, the His-tags on the enzyme were removed using thrombin. rBlmet was then applied to MiaPaCa- 2 cells, and the cell viability of MiaPaCa-2 cells was evaluated by neutral red assay after rBlmet treatment. The combined effect of etoposide with rBlmet against MiaPaCa-2 cells was also evaluated for 12 and 24 hours using a neutral red assay. Furthermore, cell morphology was evaluated by Giemsa and DAPI/F-actin staining methods. Survivin and caspase-3 gene expression levels were measured by RT-qPCR.</p><p><strong>Results and discussion: </strong>The specific activity of the enzyme increased after His-tag elimination to 5.62 μmol/mg per minute. rBlmet showed a significant cytotoxic effect on the MiaPaCa-2 cell line. The IC<sub>50</sub> value (24 h) of rBlmet for MiaPaCa-2 cells was 3.02 U/mL. In addition, rBlmet increased the cytotoxic effect of etoposide on the MiaPaCa-2 cell line, while it showed less effect on HaCat, which is a normal human cell line. Furthermore, rBlmet increased caspase-3 expression and downregulated survivin gene expression in MiaPaCa-2 cell lines. It successfully inhibited the growth of Mia-PaCa-2 cells by exploiting exogenous methionine amino acid in the growth medium. This study revealed promising results. However, further studies are needed on additional pancreatic cancer cell lines and <i>in vivo</i> models.</p><p><strong>Conclusion: </strong>Based on these findings, it can be concluded that rBlmet not only has great potential to treat pancreatic cancer in the future but can also be used as an adjuvant to enhance the effectiveness of chemotherapeutic agents like etoposide.</p>","PeriodicalId":20736,"journal":{"name":"Protein and Peptide Letters","volume":" ","pages":"451-464"},"PeriodicalIF":1.1,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144560879","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Evaluation of the Anti-Liver Cancer Activity of Protein Fractions Isolated from <i>Adenium obesum</i> Leaf Extract.","authors":"Ashkan Hajinourmohammadi, Jamil Zargan, Hanieh Jafary, Firouz Ebrahimi","doi":"10.2174/0109298665411024251015093155","DOIUrl":"10.2174/0109298665411024251015093155","url":null,"abstract":"<p><strong>Introduction: </strong>Liver cancer is the third leading cause of cancer-related death. Plantderived therapeutics have played a significant role in preventing and treating many diseases, including cancers. The present study investigated the anticancer properties of protein fractions from the green leaf extract of <i>Adenium obesum</i> (A. obesum) in the laboratory.</p><p><strong>Methods: </strong>Protein fractions of leaf extract were separated using reversed-phase high-performance liquid chromatography (RP-HPLC). The cytotoxicity of protein fractions was studied by MTT and sulforhodamine B assays. The apoptotic cell death was examined using the alkaline comet assay, and redox-related indicators were assessed using the catalase enzyme activity assay, glutathione content, and nitric oxide release. The RBC hemagglutination test investigated the possible presence of ribosome-inactivating proteins (RIPs) in the most toxic protein fraction, and the LD50 of the protein fraction with the highest anticancer effects was determined. The amino acid sequence of fraction proteins was determined by the matrix-assisted laser desorption ionization-time of flight mass spectrometry (MALDI-TOF MS) method.</p><p><strong>Results: </strong>The results showed that protein fraction 8 had the highest toxicity in the HepG2 cell line, with an IC<sub>50</sub> of 0.16 μg/mL. This fraction induced hemagglutination in red blood cells at concentrations higher than 65 μg/mL. The apoptosis was induced in the HepG2 cells following treatment with the concentrations of 0.08, 0.16, 0.32, and 0.64 μg/mL. Moreover, the redox potential of the treated cells was changed after treatment. The <i>in vivo</i> cytotoxicity investigation of this fraction in mice showed that it is not toxic for animals in concentrations up to 800 μg/kg, indicating its safety potential for pharmaceutical applications. The protein extract in the aforementioned fraction contained two proteins (22 and 53 kD) as determined by electrophoresis and sequencing methods.</p><p><strong>Conclusion: </strong>The findings of this investigation demonstrated that the protein content of fraction 8 derived from A. obesum leaf extract possesses anticancer activity in the HepG2 cell line. The two isolated proteins from this fraction are novel and have been reported for the first time. Further investigations should be performed to evaluate the treatment potential in in vitro/vivo conditions.</p>","PeriodicalId":20736,"journal":{"name":"Protein and Peptide Letters","volume":" ","pages":"742-755"},"PeriodicalIF":1.1,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145438969","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"ZNF165: A Pan-Cancer Biomarker with Prognostic and Therapeutic Potential.","authors":"Guizhen Lyu, Dongbing Li","doi":"10.2174/0109298665351592250106062250","DOIUrl":"10.2174/0109298665351592250106062250","url":null,"abstract":"<p><strong>Background: </strong>The role of ZNF165 in only a few tumors has been reported. ZNF165 plays an important role in liver cancer, gastric cancer, and breast cancer, especially in regulating the immune microenvironment, promoting tumor cell proliferation and migration, and serving as a potential target for immunotherapy.</p><p><strong>Objective: </strong>This study aimed to enhance an understanding of how the ZNF165 gene functions and influences cancer development.</p><p><strong>Methods: </strong>Using a suite of online resources, including TIMER, TCGA, GTEx, GEPIA2, cBioPortal, TIMER2, STRING, DAVID, RNAactDrug, CancerSEA, and UCSC, along with comprehensive statistical analyses, we conducted a thorough investigation of the pan-cancer landscape of ZNF165. This study encompassed an assessment of ZNF165 levels, their associations with patient outcomes, and clinical correlates. We examined the interplay between ZNF165 and key cancer biomarkers, such as Microsatellite Instability (MSI), Tumor Mutational Burden (TMB), immune cell infiltration, and the expression of immune checkpoint genes. We delved into the genetic variations of ZNF165, its biological roles across various cancer types, and its potential links to drug responsiveness. We analyzed single-cell expression patterns of ZNF165 and their implications for the functional dynamics of cancer. We employed quantitative Reverse Transcription PCR (qRT-PCR) to measure ZNF165 levels in Ovarian Cancer (OC) cell lines.</p><p><strong>Results: </strong>ZNF165 expression displayed aberrations across a diverse range of human cancers and exhibited correlations with clinical stages. High ZNF165 expression in KIRC, KIRP, STAD, and UCEC was significantly associated with poor overall survival. ZNF165 has encouraging diagnostic value in specific tumor types, with gene amplification identified as the predominant genetic alteration. Our analysis further uncovered significant associations between ZNF165 levels and MSI across three distinct cancer types, as well as with TMB in six different malignancies. We detected substantial correlations between ZNF165 levels and immune cell infiltration, as well as the expression of immune checkpoint genes. ZNF165 was found to be involved in several prevalent signaling pathways across various cancer types. ZNF165 may potentially contribute to chemotherapy and chemoresistance, and was observed to be involved in cancer progression. A ceRNA regulatory network involving AFDN-DT, miR-191-5p, and ZNF165 was constructed for OC, revealing significantly elevated ZNF165 levels in OC cell lines. Dysregulated ZNF165 expression across a spectrum of malignancies might play a role in cancer initiation and advancement via multiple biological pathways.</p><p><strong>Conclusion: </strong>ZNF165 may serve as a promising therapeutic target for the treatment of cancer in human patients.</p>","PeriodicalId":20736,"journal":{"name":"Protein and Peptide Letters","volume":" ","pages":"206-223"},"PeriodicalIF":1.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143047661","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Recombinant Production of Ib-AMP<sub>4</sub> and Oncorhyncin II Antimicrobial Peptides and Antimicrobial Synergistic Assessment on the Treatment of <i>Staphylococcus aureus</i> Under <i>In vitro</i> Condition.","authors":"Majid Safari, Hamid Abtahi, Shima Chehreii, Shohreh Fahimirad","doi":"10.2174/0109298665327474241112093601","DOIUrl":"10.2174/0109298665327474241112093601","url":null,"abstract":"<p><strong>Background: </strong>Methicillin-resistant <i>Staphylococcus aureus</i> (MRSA) is a significant and prevalent pathogen that poses a major challenge in healthcare environments. In light of the growing threat posed by multidrug-resistant organisms like MRSA, there is an urgent need for alternative therapeutic strategies. One promising avenue of research involves the use of antimicrobial peptides (AMPs). These naturally occurring molecules, which are part of the innate immune response in many organisms, have garnered attention for their ability to combat a wide range of pathogens.</p><p><strong>Objectives: </strong>This study aimed to produce recombinant versions of Ib-AMP<sub>4</sub> and Oncorhyncin II and to evaluate their combined effects against MRSA (NCTC10442).</p><p><strong>Methods: </strong><i>Escherichia coli BL21(DE<sub>3</sub>)</i> served as the expression host for the synthesized variants of the Ib-AMP<sub>4</sub> and Oncorhyncin II genes. The antimicrobial efficacy of these peptides against MRSA <i>S. aureus</i> (NCTC1042) was evaluated using a comprehensive methodology that encompassed the determination of the minimum inhibitory concentration (MIC), the performance of time-kill assays, and the analysis of growth kinetics.</p><p><strong>Results: </strong>The individual antimicrobial activities of Ib-AMP<sub>4</sub> and Oncorhyncin II were assessed, revealing minimum inhibitory concentrations (MICs) of 27.75 μg/mL and 40.125 μg/mL against S. aureus (MRSA) (NCTC10442), respectively. The application of a checkerboard assay to evaluate the combination of these antimicrobial peptides (AMPs) demonstrated a synergistic interaction, which was further validated through time-kill and growth kinetic studies. When administered at double the MIC, a significant reduction in the log<sub>10</sub> CFU/mL of MRSA (NCTC 10442) was observed, underscoring the synergistic bacteriostatic effect mediated by the fractional inhibitory concentration (FIC) index of the two peptides.</p><p><strong>Conclusion: </strong>Antimicrobial peptides (AMPs) have attracted significant interest owing to the growing intricacy of microbial infections. They constitute a promising category of novel antibiotics that warrant further investigation for the treatment of <i>S. aureus</i> infections and the enhancement of wound healing. Although certain AMPs can operate autonomously, others may necessitate a synergistic approach alongside conventional antibiotics. Studies examining the combined efficacy of Oncorhyncin II and Ib-AMP<sub>4</sub> against MRSA <i>in vitro</i> have revealed their effectiveness.</p>","PeriodicalId":20736,"journal":{"name":"Protein and Peptide Letters","volume":" ","pages":"34-43"},"PeriodicalIF":1.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142732170","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Customizing Proteins: Reassigning Functionality of Proteins <i>via</i> Incorporation of Unnatural Amino Acids.","authors":"Maharsh Jayawant, Nagarajan Kayalvizhi, Muthukalingan Krishnan, Santhoshkumar Aruni Wilson, Neelamegam Rameshkumar","doi":"10.2174/0109298665417414251007054305","DOIUrl":"10.2174/0109298665417414251007054305","url":null,"abstract":"<p><p>The natural horizon of the genetic code has expanded to incorporate amino acids, such as selenocysteine and pyrrolysine. Researchers have incorporated unnatural amino acids (UAAs) into target proteins, demonstrating increased protein functionality depending on their choice and target. The primary challenge in protein engineering is identifying novel antimicrobial short peptides effective against ESKAPE pathogens (Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, and Enterobacter spp.), which are categorized as multidrug-resistant (MDR). UAAs can be preferentially incorporated into short peptides to display therapeutic activity, potentially leading to next-generation targeted therapeutics. In purview of this, we have curated and summarized the applicability of genetic incorporations of UAAs in antimicrobial short peptides with a special emphasis on the importance of green synthesis. The approach affirmed a reduction in the toxicity of peptide drugs, making it biocompatible. This is an efficient protocol to develop novel antimicrobial short peptides catering to precision medications, particularly against MDR pathogens, as a sustainable pharmaceutical approach.</p>","PeriodicalId":20736,"journal":{"name":"Protein and Peptide Letters","volume":" ","pages":"769-771"},"PeriodicalIF":1.1,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145346651","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Virtual Screening of Phytoconstituents in Indian Spices based on their Inhibitory Potential against SARS-CoV-2.","authors":"Vaishali Singh, Aliza Rabbani, Veda P Pandey","doi":"10.2174/0109298665366911250416113831","DOIUrl":"10.2174/0109298665366911250416113831","url":null,"abstract":"<p><strong>Background: </strong>COVID-19 is caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), a highly pathogenic human coronavirus (CoV). For the treatment of COVID-19, various drugs, ayurvedic formulations, used for other diseases, were repurposed. Ayurveda and yoga exhibited a pivotal role in the treatment of COVID-19. Various medicinal plants, including garlic, tulsi, clove, cinnamon, ginger, black pepper, and turmeric, are recommended for the prevention of COVID-19 as immunity boosters along with their antiviral property.</p><p><strong>Objective: </strong>In view of the drug repurposing approach, the present work has been initiated with the broader objectives of screening and identification of phytoconstituents of Indian spices against targets, namely furin, 3C-like protease (3CL-PRO), NSP-9 RNA binding protein, papain-like protease, RNA dependent RNA polymerase (RDRP), spike protein concerned with life cycle of SARS-CoV-2 using in-silico tools.</p><p><strong>Methods: </strong>The phytoconstituents of Indian spices were screened for interaction with several targets using a molecular docking approach with the help of Discovery Studio 4.5 software. Furthermore, the pharmacokinetic analyses of selected ligands using ADMET and Lipinski's rule of five were also performed.</p><p><strong>Results: </strong>In the present study, a total of 37 active phytoconstituents of Indian spices were screened for interaction with several identified targets of COVID-19 using a molecular docking approach. The ligands, namely morin, gingerol, myristic acid, quercetin, gallic acid and alliin were found to be the top interacting ligands with the targets analyzed.</p><p><strong>Conclusion: </strong>Based on the present <i>in-silico</i> finding, the active components of spices could be considered for drug-lead compounds against COVID-19.</p>","PeriodicalId":20736,"journal":{"name":"Protein and Peptide Letters","volume":" ","pages":"335-352"},"PeriodicalIF":2.5,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144008456","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Maria Carolina Oliveira de Arruda Brasil, Cleverson Rogerio Princival, Vinicius Kuchenbecker, Edson Katekawa, Wagner Vidal Magalhaes, Eduardo Maffud Cilli
{"title":"Deprotection Bases as an Alternative to the Traditional Bases Used in Solid-Phase Peptide Synthesis.","authors":"Maria Carolina Oliveira de Arruda Brasil, Cleverson Rogerio Princival, Vinicius Kuchenbecker, Edson Katekawa, Wagner Vidal Magalhaes, Eduardo Maffud Cilli","doi":"10.2174/0109298665421169251017073843","DOIUrl":"10.2174/0109298665421169251017073843","url":null,"abstract":"<p><strong>Background: </strong>The use of peptides in the pharmaceutical and cosmetic industries is attracting increasing attention. Most of the peptides currently marketed are obtained by chemical processes, most frequently solid-phase peptide synthesis (SPPS).</p><p><strong>Objective: </strong>Although SPPS is efficient, it requires hazardous solvents, such as N,N-dimethylformamide, dichloromethane, and N-methylpyrrolidone, as well as the bases piperidine and 4-methylpiperidine in the deprotection step. This study presents two alternative reagents, 2-aminoethanol and 2-amino-2-methyl-1- propanol, for the removal of the fluorenyl-methyloxycarbonyl protecting group used in SPPS.</p><p><strong>Methods: </strong>The traditional and alternative green SPPS using Fmoc protocol were employed.</p><p><strong>Results: </strong>The synthesis of two peptides showed that the 2-aminoethanol and 2-amino-2-methyl-1-propanol are viable replacements for piperidine-derived reagents in peptide synthesis.</p><p><strong>Discussion: </strong>The use of these reagents in SPPS afforded two peptides in high yield in an environmentally sustainable solvent.</p><p><strong>Conclusion: </strong>The reagents are thus promising alternatives to piperidine derivatives, particularly 2-amino- 2-methyl-1-propanol, in SPPS.</p>","PeriodicalId":20736,"journal":{"name":"Protein and Peptide Letters","volume":" ","pages":"836-841"},"PeriodicalIF":1.1,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145452566","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}